Lutein and zeaxanthin, prominent carotenoids with antioxidant properties, contribute
notably to maintaining of ocular health. These substances reduce the harmful effect
of oxidative stress and blue light and ensure the vision quality. Carotenoids-rich
dietary could have ophthalmic benefits, such as enhanced contrast perception and reduced
eye fatigue, while also show potential in mitigating the risk of age-related macular
degeneration (AMD). Nonetheless, ocular administration of carotenoids could enhance
the local ophthalmic bioavailability of these compounds. The aim of this study was
to investigate ophthalmic applicability of lutein (LutD) and zeaxanthin disuccinates
(ZeaD) in aqueous solutions applying cyclodextrins to improve their solubility and
permeability. Among the tested cyclodextrins, randomly methylated beta-cyclodextrin
(RAMEB) was identified as the most effective solubilizing agent, achieving solubility
values of 572±55 μM and 1470±103 μM for LutD and ZeaD, respectively. In vitro corneal-PAMPA
and ex vivo porcine eye models demonstrated that RAMEB-based formulations significantly
improved the permeability of both carotenoid derivatives by increasing their solubility
(corneal concentration at 15 mins), markedly surpassing those of the reference suspensions.
The findings suggest that RAMEB may be essential for developing carotenoid-based aqueous
eye drops, leveraging its antioxidant properties to improve ocular health and ameliorate
various degenerative eye conditions.
